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Assay Detail

CHEMBL873207

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of 3'- processing activity of HIV-1 integrase
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Human immunodeficiency virus type 1 integrase (CHEMBL3471)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Curcumin analogs with altered potencies against HIV-1 integrase as probes for biochemical mechanisms of drug action.
Mazumder A, Neamati N, Sunder S, Schulz J, Pertz H, Eich E, Pommier Y.
J Med Chem (1997) 40 : 3057 -3063
PubMed 9301668 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.01 5.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL319488 DIDEMETHYLCURCUMIN 1 5.22
CHEMBL324842 ROSMARINIC ACID 1 5.05
CHEMBL103410 1 4.75
CHEMBL140 CURCUMIN 3.0 1 -
CHEMBL105350 BISDEMETHOXYCURCUMIN 1 -
CHEMBL103006 1 -
CHEMBL179512 DEMETHOXYCURCUMIN 1 -
CHEMBL102914 1 -
CHEMBL318743 TETRAHYDROCURCUMIN 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL319488 DIDEMETHYLCURCUMIN IC50 = 6000.0 nM 5.22
CHEMBL324842 ROSMARINIC ACID IC50 = 9000.0 nM 5.05
CHEMBL103410 IC50 = 18000.0 nM 4.75
CHEMBL140 CURCUMIN IC50 = 150000.0 nM -
CHEMBL105350 BISDEMETHOXYCURCUMIN IC50 = 120000.0 nM -
CHEMBL103006 IC50 > 300000.0 nM -
CHEMBL179512 DEMETHOXYCURCUMIN IC50 = 140000.0 nM -
CHEMBL102914 IC50 > 300000.0 nM -
CHEMBL318743 TETRAHYDROCURCUMIN IC50 > 300000.0 nM -